✦ LIBER ✦

Cover Picture: 2-Anilinobenzamides as SIRT Inhibitors (ChemMedChem 10/2006)

✍ Scribed by Takayoshi Suzuki; Keiko Imai; Hidehiko Nakagawa; Naoki Miyata

Book ID: 102100627
Publisher: John Wiley and Sons
Year: 2006
Tongue: English
Weight: 35 KB
Volume: 1
Category: Article
ISSN: 1860-7179
DOI: 10.1002/cmdc.200690035

No coin nor oath required. For personal study only.

✦ Synopsis

The cover picture shows the model of a SIRT inhibitor, 2‐anilinobenzamide, bound to the catalytic core of a SIRT homologue. SIRTs catalyze the deacetylation of several proteins such as histones, p53, and γ‐tubulin, and are involved in certain disease states including cancer. SIRT inhibitors can be considered as potential therapeutic agents. This simple compound, which was discovered from a nicotinamide‐ and benzamide‐focused chemical library, shows potent SIRT1 inhibition competitive with the acetylated lysine substrate and causes p53 acetylation in human colon cancer HCT116 cells. For more details, see the Communication by T. Suzuki, N. Miyata et al. on p. 1059 ff.

📜 SIMILAR VOLUMES

Cover Picture: Synthesis and Evaluation

Cover Picture: Synthesis and Evaluation of 3,4-Dihydropyrimidin-2(1 H )-ones as Sodium Iodide Symporter Inhibitors (ChemMedChem 1/2013)

✍ Lacotte, Pierre; Puente, Celine; Ambroise, Yves 📂 Article 📅 2012 🏛 John Wiley and Sons 🌐 English ⚖ 854 KB

Cover Picture: Urolithin as a Converging

Cover Picture: Urolithin as a Converging Scaffold Linking Ellagic acid and Coumarin Analogues: Design of Potent Protein Kinase CK2 Inhibitors (ChemMedChem 12/2011)

✍ Dr. Giorgio Cozza; Dr. Alessandra Gianoncelli; Dr. Paolo Bonvini; Dr. Elisa Zorz 📂 Article 📅 2011 🏛 John Wiley and Sons 🌐 English ⚖ 778 KB

The cover picture shows the hypothetical binding motif of a novel potent protein kinase CK2 inhibitor, 4-bromo-3,8-dihydroxy-benzo[c]chromen-6-one, which shows a K i value of 7 nm. CK2 is a ubiquitous, essential, and highly pleiotropic protein kinase, and abnormally high constitutive activity of thi

Cover Picture: Identification of Selecti

Cover Picture: Identification of Selective Inhibitors of the Potassium Channel Kv1.1–1.2(3) by High-Throughput Virtual Screening and Automated Patch Clamp (ChemMedChem 10/2012)

✍ Sören J. Wacker; Dr. Wiktor Jurkowski; Dr. Katie J. Simmons; Prof. Dr. Colin W. 📂 Article 📅 2012 🏛 John Wiley and Sons 🌐 English ⚖ 729 KB

Cover Picture: 2,3-Dihydro-1-Benzofuran

Cover Picture: 2,3-Dihydro-1-Benzofuran Derivatives as a Series of Potent Selective Cannabinoid Receptor 2 Agonists: Design, Synthesis, and Binding Mode Prediction through Ligand-Steered Modeling (ChemMedChem 10/2009)

✍ Philippe Diaz; Sharangdhar S. Phatak; Jijun Xu; Frank R. Fronczek; Fanny Astruc- 📂 Article 📅 2009 🏛 John Wiley and Sons 🌐 English ⚖ 972 KB